Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1987-02-13
1988-08-30
Phillips, Delbert R.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
530302, 564157, 514616, 514423, 548537, 548538, A61K 3702, C07K 506, C07C10320, C07D20700
Patent
active
047677449
ABSTRACT:
This invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable addition salts thereof, wherein R.sup.1 is --OH, --OCH.sub.3 or lower alkoxy of 1-6 carbon atoms; wherein R.sup.2 and R.sup.3 may be the same or different and represent straight or branched chain lower alkyl of 1-6 carbon atoms; wherein R.sup.4, R.sup.5 R.sup.9 may be the same or different and represent hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; wherein R.sup.6 represents hydrogen, or straight or branched chain lower alkyl of 1-6 carbon atoms, or R.sup.6 may act together with N.sup.6, C.sup.w and either R.sup.7 R.sup.8 to form a cycloamine of the formula: ##STR2## such that between R.sup.7 and R.sup.8, when one acts to form said cycloamine, the other is hydrogen, or straight or branched chain lower alkyl of 1-6 carbon atoms; wherein when neither R.sup.7 nor R.sup.8 is acting to form said cycloamine, R.sup.7 R.sup.8 act together with C.sup.w to form a cycloalkyl of the formula: ##STR3## where n=3, 4, 5; wherein C.sup.w represents an asymmetric carbon atom when R.sup.7 and R.sup.8 are not the same and may be racemic or have the D or L configuration; and wherein C.sup.v represents an asymmetric carbon atom that may be racemic or that may hve the D or L configuration.
These compounds are useful because they possess analgesic activity in mammals.
REFERENCES:
patent: 4127535 (1978-11-01), Coy et al.
patent: 4316892 (1982-02-01), Jones
patent: 4407746 (1983-10-01), Mazur et al.
patent: 4579841 (1986-04-01), Stewart et al.
patent: 4603121 (1986-07-01), Hansen, Jr. et al.
Clare Michael
Hansen, Jr. Donald W.
Pilipauskas Daniel R.
G. D. Searle & Co.
Grassler Frank P.
Keane J. Timothy
Matukaitis Paul D.
Phillips Delbert R.
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